Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues

Research output: Contribution to journalArticle

  • External authors:
  • Binto Simon
  • Claire Walmsley
  • Victoria J. Jackson
  • Edward P. Garvey
  • Martin J. Slater
  • David J. Berrisford

Abstract

Synthetic neamine mimetics have been evaluated for binding to the HIV-1 Rev response element. Modified neamine derivatives, obtained from reductive amination of neamine, led to identification of new 6-amino modified neamine-type ligands with HIV-1 RRE binding affinity up to 20× that of neamine and up to 6× that of the more complex neomycin itself. This provides a noteworthy structure-activity increase and a useful lead to simplified, chemically accessible mimetics.

Bibliographical metadata

Original languageEnglish
JournalBioorganic & medicinal chemistry letters
Early online date9 Nov 2018
DOIs
Publication statusPublished - 2018